Lipopeptide with a RGDK tetrapeptide sequence can selectively target genes to proangiogenic alpha5beta1 integrin receptor and mouse tumor vasculature.
Integrins, the major class of alphabeta heterodimeric transmembrane glycoprotein receptors, play crucial roles in mediating tumor angiogenesis. Genetic ablation experiments combined with use of antibodies/peptide ligands for blocking either alpha(5) or beta(1) integrins have convincingly demonstrated alpha(5)beta(1) integrin to be unquestionably proangiogenic among the 24 known integrin receptors. Herein, we report on a novel RGDK-lipopeptide 1 that targets selectively alpha(5)beta(1) integrin and is capable of targeting genes to mouse tumor vasculatures.
Pramanik
Dipankar
D
Division of Lipid Science and Technology, Pharmacology Division, Indian Institute of Chemical Technology, Hyderabad 500607, India.
Majeti
Bharat K
BK
Mondal
Goutam
G
Karmali
Priya P
PP
Sistla
Ramakrishna
R
Ramprasad
Obula G
OG
Srinivas
Gunda
G
Pande
Gopal
G
Chaudhuri
Arabinda
A
D000818:Animals; D042783:Endothelial Cells / Q000187:drug effects / Q000378:metabolism; D039081:Integrin alpha5beta1 / Q000037:antagonists & inhibitors* / Q000235:genetics* / Q000378:metabolism; D055666:Lipopeptides / Q000138:chemical synthesis / Q000737:chemistry* / Q000494:pharmacology*; D051379:Mice; D008810:Mice, Inbred C57BL; D015394:Molecular Structure; D009389:Neovascularization, Pathologic / Q000188:drug therapy / Q000235:genetics*
D039081:Integrin alpha5beta1; D055666:Lipopeptides